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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
1443 Results for "
weak
" in MedChemExpress (MCE) Product Catalog:
Products (1443)
1443 Results for "weak" in MCE Product Catalog:
Cat. No.: HY-111124
CAS No.: 923932-43-8
Synonyms: BRL29060-d2
Cat. No.: HY-114421R
CAS No.: 2064175-41-1
Synonyms: dTAG-13 (Standard)
Research Areas:
FKBP12 PROTAC dTAG-13 (Standard) is the analytical standard of FKBP12 PROTAC dTAG-13 (HY-114421). This product is intended for research and analytical applications. FKBP12 PROTAC dTAG-13 (dTAG-13) is a FKBP12 F36V PROTAC degrader and a PXR partial agonist. FKBP12 PROTAC dTAG-13 induces ubiquitination and proteasomal degradation of proteins tagged with FKBP12 F36V, without degrading wild-type FKBP12 or un-fused PXR. It weakly promotes the recruitment of SRC-1, strongly inhibits the interaction between NCoR and PXR, and upregulates the expression of CYP3A4 and other drug metabolism-related genes. FKBP12 PROTAC dTAG-13 is applicable to research related to breast cancer and leukemia .
Cat. No.: HY-122272R
CAS No.: 61869-08-7
Synonyms: BRL29060 (Standard)
Target:
Reference Standards Cytochrome P450 5-HT Receptor NO Synthase Apoptosis Serotonin Transporter Estrogen Receptor/ERR
Research Areas:
Paroxetine (BRL29060) (Standard) is the analytical standard of Paroxetine (HY-122272). This product is intended for research and analytical applications. Paroxetine (BRL29060) is an orally active and selective serotonin reuptake inhibitor (SSRI) and apoptosis inducer with blood-brain barrier permeability. Paroxetine inhibits nitric oxide synthase and CYP2D6, induces desensitization of 5-HT1A/1B/1D autoreceptors, downregulates 5-HT2 receptors, and promotes the production of inflammatory cytokines. Paroxetine is a weak norepinephrine (NE) uptake inhibitor and possesses antitumor activity. Paroxetine is widely used in research concerning depression, obsessive-compulsive disorder, panic disorder, social phobia, generalized anxiety disorder, post-traumatic stress disorder, premenstrual dysphoric disorder, hot flashes, and related conditions .
Cat. No.: HY-122272S
CAS No.: 923932-45-0
Synonyms: BRL29060-d4
Cat. No.: HY-123859
CAS No.: 1454584-91-8
Target:
Research Areas:
SR-2890 is a highly selective, ATP-competitive inhibitor of casein kinase CK1δ and CK1ε, with IC50 values of 4 nM and 44 nM, respectively, and a Ki of 14 nM for CK1δ. SR-2890 exhibits antiproliferative effects. SR-2890 blocks the serine/threonine kinase activity of CK1δ and weakly inhibits a few off-target kinases such as FLT3, CDK4. SR-2890 has an oral bioavailability of 10% and a blood-brain barrier penetration rate of <1%. SR-2890 demonstrates stable in vitro metabolism and favorable in vivo pharmacokinetic properties, effectively inhibiting the growth of human A375 melanoma cells. SR-2890 can be used in melanoma research and is also a useful compound for studying CK1δ/ε-related diseases such as Alzheimer's disease .
Synonyms: ABT-301; MPT0E028; TMU-C-0012
Research Areas:
Imofinostat (ABT-301; MPT0E028) is an orally active and selective HDAC inhibitor with IC50s of 53.0 nM, 106.2 nM, 29.5 nM for HDAC1, HDAC2 and HDAC6, respectively. Imofinostat has a weak inhibitory effect on HDAC8 (IC50 of 2.5 μM), but no inhibitory effect on HDAC4 (IC50>10 μM). Imofinostat reduces the viability of B-cell lymphomas by inducing apoptosis and possesses potent direct Akt targeting ability and reduces Akt phosphorylation in B-cell lymphoma. Imofinostat has a broad-spectrum antitumor activity, including colorectal cancer, B-cell lymphoma, non-small cell lung carcinoma (NSCLC), and pancreatic cancer, while also showing therapeutic potential in non-tumor diseases like emphysema and pulmonary fibrosis .
Cat. No.: HY-143797S
Cat. No.: HY-165624B
CAS No.: 136296-43-0
Target:
Research Areas:
(R)-LY-41, R-enantiomer of LY-41 (HY-165624), is 2-Sminotetralin (HY-W022362) derivative and 8-OH-DPAT (HY-112061) analogue. (R)-LY-41 is a potent and selective 5-HT1A receptor agonist. (R)-LY-41 can reduce the accumulation of 5-hydroxytryptophan (the precursor for 5-HT synthesis) in the rat brain induced by decarboxylase inhibitors (NSD 1015). (R)-LY-41 can lower the body temperature of rats and inhibit the escape response from the cage. (R)-LY-41 can induce the 5-HT behavioral syndrome but is weaker than (S)-LY-41 (HY-165624A). (R)-LY-41 can be used for the research of neurological disease, such as depression and anxiety .
Cat. No.: HY-17357S
CAS No.: 1246814-53-8
Synonyms: AHR-9434-d5; AL-6515-d5
Cat. No.: HY-174301
CAS No.: 3052223-40-9
Research Areas:
USP7-IN-18 is a naphthalene derivative. USP7-IN-18 is a selective USP7 inhibitor (IC50 : 130.9 nM), with no or very weak inhibition of the other 8 DUBs including USP47. USP7-IN-18 specifically binds to the catalytic domain of USP7, blocking its deubiquitinase activity. USP7-IN-18 causes degradation of the oncogenic proteins MDM2 and DNMT1, and also degrades the novel target PCLAF. USP7-IN-18 activates the p53-p21 pathway. USP7-IN-18 exerts anti-tumor effects in colon cancer animal models and reshapes the tumor immune microenvironment. USP7-IN-18 achieves both direct cytotoxic and immune-synergistic anti-tumor actions.
Cat. No.: HY-180811
Research Areas:
ALK/HDAC-IN-2 (Compound 19b) is an ALK/HDAC inhibitor with IC₅₀ values for ALK WT and total HDACs of 8 nM and 1.18 μM, respectively. ALK/HDAC-IN-2 exhibits inhibitory activity against ALK mutants G1202R, F1174L, and L1196M, with IC₅₀ values of 2.74, 9.23, and 34.28 nM, respectively. ALK/HDAC-IN-2 shows potent and selective inhibition against HDAC1 (IC₅₀ = 0.24 μM), while its inhibitory activity against HDAC7, HDAC6, and HDAC11 is weak (IC₅₀ > 10 μM). ALK/HDAC-IN-2 has broad-spectrum anti-proliferative activity against various cancer cells, inducing cell cycle arrest and apoptosis. ALK/HDAC-IN-2 can be used for the study of neuroblastoma .
Cat. No.: HY-183399
CAS No.: 95669-35-5
Target:
Research Areas:
Wy 27127 is a potent and selective α2-adrenergic receptor antagonist. Wy 27127 competitively blocks α2-adrenergic receptors, interrupts the negative feedback loop of sympathetic nerve endings, enhances stimulus-evoked norepinephrine release, and blocks agonist-induced inhibition of vas deferens contraction. Wy 27127 shows weak antagonistic effects on α1 receptors, and exhibits no significant antagonistic activity against 5-hydroxytryptamine, muscarinic, presynaptic dopamine, histamine or β1-adrenergic receptors in vitro. Wy 27127 blocks saphenous vein contraction mediated by postsynaptic α2-adrenergic receptor agonists. Wy 27127 is applicable to studies related to sympathetic neurotransmission and vascular adrenergic responses .
Cat. No.: HY-184335
CAS No.: 3097564-20-7
Research Areas:
PROTAC BET Degrader-18 is a PROTAC targeting BET, with a DC50 of 0.676 nM in HEK293-BRD4-HiBiT-KI cells. PROTAC BET Degrader-18 mainly targets and degrades BRD4 (EC50 = 59.91 nM), and exhibits weak degradation activity against BRD2. PROTAC BET Degrader-18 inhibits the expression of downstream oncoprotein c-Myc, thereby inducing cell cycle arrest and apoptosis, while suppressing oncoprotein expression. PROTAC BET Degrader-18 shows antiproliferative activity against acute myeloid leukemia cells and triple-negative breast cancer cells. PROTAC BET Degrader-18 demonstrates antitumor efficacy in xenograft mouse models. PROTAC BET Degrader-18 can be used for the research of acute myeloid leukemia and triple-negative breast cancer .
Cat. No.: HY-B0383AS
CAS No.: 1794782-57-2
Synonyms: PNU180638 hydrochloride-d6
Cat. No.: HY-B0383AS2
Synonyms: PNU180638 free base-d3 benzoate
Cat. No.: HY-N19899
CAS No.: 910050-51-0
Category:
Target:
Synonyms: MK-678; L-363586
Target:
Cat. No.: HY-122272S2
CAS No.: 1435728-63-4
Synonyms: BRL29060-d6-1
Cat. No.: HY-156807
CAS No.: 210751-39-6
Target:
Research Areas:
LY 367265 is a 5-hydroxytryptamine transporter (SERT) inhibitor (IC₅₀ = 3.1 nM) and a 5-HT₂A receptor antagonist (Kᵢ = 0.81 nM). LY 367265 has the inhibitory activity on the norepinephrine transporter (NET) of extremely weak (IC₅₀ > 1000 nM); it has low affinity for subtypes such as 5-HT₁B (Kᵢ = 490 nM) and 5-HT₁D (Kᵢ = 81 nM), showing high selectivity. LY 367265 concentration-dependently enhances of [³H]5-HT efflux (EC₅₀ = 250 nM). LY 367265 antagonizes the contraction response of Sumatriptan (HY-B0121B), indicating its functional antagonistic activity on 5-HT₁D-like receptors. LY 367265 can be used for the study of diseases such as anxiety disorders and post-traumatic stress disorder .
Cat. No.: HY-162240
Target:
Research Areas:
SJH1-51B is a SKP1-recruiting BRD4 PROTAC degrader. SJH1-51B binds to SKP1 in the SKP1-FBXO7-CUL1-RBX1 complex, but shows no or weak binding to monomeric SKP1. SJH1-51B induces proteasome- and SKP1-dependent degradation of BRD4, and this degradation process relies on the neddylation modification of Cullin-RING E3 ligase. SJH1-51B induces proteasome-mediated degradation of the short isoform of BRD4 in non-cancer cells, while it induces proteasome-mediated degradation of both the long and short isoforms of BRD4 in breast cancer cells. SJH1-51B can be used for breast cancer research .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
